P
US8772247B2ActiveUtilityPatentIndex 41

Anti-parasitic compounds

Assignee: LININGTON ROGERPriority: Mar 20, 2009Filed: Mar 20, 2010Granted: Jul 8, 2014
Est. expiryMar 20, 2029(~2.7 yrs left)· nominal 20-yr term from priority
Inventors:LININGTON ROGERSANCHEZ LAURA
A61K 38/08A61P 33/02C07K 7/06A61K 38/00A61K 31/555A61K 31/155A61K 31/185Y02A50/30A61P 33/00
41
PatentIndex Score
0
Cited by
4
References
4
Claims

Abstract

A novel structural class of highly N-methylated linear lipopeptide compounds useful for the treatment of parasitic disease.

Claims

exact text as granted — not AI-modified
The invention claimed is: 
     
       1.  1  An almiramide molecule, comprising a linear lipopeptide having the following structure 
       
         
           
           
               
               
           
         
         but specifically excluding compounds (1), (2) and (3) 
         wherein for (1), R 1  consists of 
       
       
         
           
           
               
               
           
         
          R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2: 
         and wherein for (2), R 1  consists of 
       
       
         
           
           
               
               
           
         
          R 2  consists of Me, R 3  consists of H, and R 4 consists of NH2; 
         and wherein for (3), R 1  consists of 
       
       
         
           
           
               
               
           
         
          R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2, and further, 
         wherein R 1  is selected from one of the following moieties: 
       
       
         
           
           
               
               
           
         
         and wherein R 2  is selected from one of the following moieties: Me or H 
         and wherein R 3  is selected from one of the following moieties: Me or H 
         and wherein R 4  is selected from one of the following moieties: NH 2  , NMe 2  , OH, OMe. 
       
     
     
       2. An almiramide molecule, comprising a linear lipopeptide having the following structure 
       
         
           
           
               
               
           
         
         but specifically excluding compounds (1), (2) and (3) 
         wherein for (1), R 1  consists of 
       
       
         
           
           
               
               
           
         
          R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2: 
         and wherein for (2), R 1  consists of 
       
       
         
           
           
               
               
           
         
          R 2  consists of Me, R 3  consists of H, and R 4  consists of NH2; 
         and wherein for (3), R 1  consists of 
       
       
         
           
           
               
               
           
         
          R 2  consists of Me, R 3  consists of H, and R4 consists of NH2, and further, wherein said almiramide molecule is selected from the group consisting of compounds 4, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, and 24 as shown below: 
       
       
         
           
                 
                 
                 
                 
                 
               
                     
                 
                   Comp. 
                   R 1   
                   R 2   
                   R 3   
                   R 4   
                 
                     
                 
                    4 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   H 
                   NH 2   
                 
                     
                 
                   11 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   Me 
                   NH 2   
                 
                     
                 
                   12 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   Me 
                   Me 
                   NMe 2   
                 
                     
                 
                   13 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   14 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   15 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   16 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   NMe 2   
                 
                     
                 
                   17 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OH 
                 
                     
                 
                   18 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OH 
                 
                     
                 
                   19 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OH 
                 
                     
                 
                   20 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OH 
                 
                     
                 
                   21 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OMe 
                 
                     
                 
                   22 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OMe 
                 
                     
                 
                   23 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                   OMe 
                 
                     
                 
                   24 
                   
                     
                       
                       
                           
                           
                       
                     
                   
                   H 
                   Me 
                    OMe. 
                 
                     
                 
             
                
                
                
               
               
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
       3. The almiramide molecule of  claim 2  comprising an N—N-dimethyl-amide C-terminus. 
     
     
       4. The almiramide molecule of  claim 2  comprising at least one unsaturated terminus.

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